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Volume 4, Issue 2 American Journal of Ethnomedicine
ISSN 2348-9502
Natural Products Congress & World Pharma Congress 2017
October 16-18, 2017
3rd World Congress on
NATURAL PRODUCTS CHEMISTRY AND RESEARCH
&
12th WORLD PHARMA CONGRESS
October 16-18, 2017 Budapest, Hungary
Anti-inflammatory effects of a PPAR-γ agonistic phthalimide analogue
Jee H Jung, Mingzhi Su, Jiafu Cao, Jin Huang, Sen Liu, Dong-Soon Im and Jin-Wook Yoo
Pusan National University, South Korea
Previously, we isolated a new compound paecilocin A as a PPAR-γ binding molecule from the jellyfish-derived fungus Paecilomyces
variotii. Based on the molecular framework of paecilocin A, a series of phthalimide analogues were synthesized and evaluated for
PPAR-γ binding activity. In a subsequent screening for competitive binding activity, 4-hydroxy-2-(4-hydroxyphenethyl) isoindoline-
1,3-dione (PD1) showedgoodPPAR-γ agonistic activity. Since one of the functions of PPAR-γ is suppressionof inflammatory responses,
the present study aimed to investigate anti-inflammatory activity of PD1. Transcriptions of mRNA were determined by reverse
transcriptase-PCR. Inflammatory protein expressions were determined by ELISA and Western blot method. In Lipopolysaccharide
(LPS)-stimulatedmurinemacrophage RAW264.7 cells, PD1 suppressed the induction of pro-inflammatory factors including inducible
Nitric Oxide Synthase (iNOS), Nitric Oxide (NO), Cyclooxygenase 2 (COX-2), Tumor Necrosis Factor α (TNF-α), interleukine 1β
(IL-1β), and interleukine 6 (IL-6) in both mRNA level and protein level. In parallel, PD1 enhanced expression of anti-inflammatory
factors such as arginase-1 and interleukine 10 (IL-10). PD1 simultaneously suppressed LPS-evoked Nuclear Factor kappa B (NF-κB)
p65 subunit phosphorylation in macrophages. The anti-inflammatory mechanism of PD1 is proposed to be via inhibition of NF-κB
pathway. In subsequent in vivo animal experiment employing carrageenan-induced acute inflammatory paw edema model, PD1
showed significant reduction in paw swelling. Histological analysis of tissue sections revealed reduction of cellular infiltration of
immune cells in PD1-treated groups. These findings suggest that PD1 may serve as an anti-inflammatory lead.
Biography
Jee H Jung has his expertise in isolation, structure elucidation, and biological evaluation of new compounds from marine organisms. In recent years, his research
was focused on the study of bioactive compounds from marine invertebrate-derived microorganisms. Further studies on optimization of lead compounds by docking
simulation-based analogue synthesis and enhancement of bioavailability by nanoparticle formulation are also his major research interests.
Jee H Jung et al., American Journal of Ethnomedicine, 4:2
DOI: 10.21767/2348-9502-C1-002